首页> 外国专利> QUINOXALINE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF HAVING MCH1R INHIBITORY ACTIVITY, PROCESS FOR PREPARATION AND USE THEREOF FOR TREATING OBESITY

QUINOXALINE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF HAVING MCH1R INHIBITORY ACTIVITY, PROCESS FOR PREPARATION AND USE THEREOF FOR TREATING OBESITY

机译:具有MCH1R抑制活性的喹喔啉衍生物及其药物可接受的盐,其制备方法及用于治疗肥胖的方法

摘要

A quinoxaline derivatives having activity of suppressing melanin-concentrating hormone 1 receptor (MCH1R) is provided to treat diseases related to obesity caused by the activation of MCH1R. A quinoxaline derivative of the chemical formula 1 has the activation of suppressing a melanin-concentrating hormone receptor (MCH1R). A method for manufacturing the quinoxaline derivative of the chemical formula 1 comprises: a first step of condensing a compound of the chemical formula 3 with 2-chloro-6-nitroquinoxaline compound of the chemical formula 2 to produce a 6-nitroquinoxaline derivative of the chemical formula 4; a second step of reducing the 6-nitroquinoxaline derivative of the chemical formula 4 to produce a 6-aminoquinoxaline derivative of the chemical formula 5; and a third step of condensing biphenyl-4-carboxylic acid compound of the chemical formula 6 with the aminoquinoxaline derivative of the chemical formula 5 to a quinoxaline derivative which 6-(biphenyl-4-carboxamido) group is substituted.
机译:提供具有抑制黑色素浓缩激素1受体(MCH1R)活性的喹喔啉衍生物,以治疗与由MCH1R的活化引起的肥胖有关的疾病。化学式1的喹喔啉衍生物具有抑制黑色素浓缩激素受体(MCH1R)的活性。化学式1的喹喔啉衍生物的制造方法包括:第一步,将化学式3的化合物与化学式2的2-氯-6-硝基喹喔啉化合物缩合,以生成化学式6的6-硝基喹喔啉衍生物。公式4;第二步,还原化学式4的6-硝基喹喔啉衍生物,得到化学式5的6-氨基喹喔啉衍生物。第三步骤是将化学式6的联苯-4-羧酸化合物与化学式5的氨基喹喔啉衍生物缩合为取代有6-(联苯基-4-甲酰胺基)基团的喹喔啉衍生物。

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